AdaAhx₃L₃VS-CAS 389064-25-9-Calbiochem

C₅₀H₈₈N₆O₈S

933.33

A cell-permeable, peptide vinyl sulfone that acts as a potent, irreversible inhibitor of proteasome activity. Covalently modifies the catalytically active β-subunits of the proteasome. Shown to inhibit the chymotrypsin-like (10-50 nM), trypsin-like (1-5 µM), and the peptidyl glutamyl peptide hydrolyzing (PGPH) (0.5-1 µM) activities of purified 20S proteasomes from rabbit muscle. Inhibits proteasomal degradation of deglycosylated MHC HLA-A2 heavy chain in US11+ cells (~50 µM).
A potent, covalent, cell-permeable, irreversible inhibitor of chymotrypsin-like (50-100 nM), trypsin-like (1-5 µM), and PGPH (0.5-1 µM) activities of the 20S proteasome.

Cell permeable: yes
Target IC₅₀: 50-100 nM against chymotrypsin-like activity of the 20S proteasome
Primary Target
chymotrypsin-like activity of the 20S proteasome
Product does not compete with ATP.
Reversible: no

Toxicity: Standard Handling (A)

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Kessler, B.M., et al. 2001. Chem. Biol.8, 913.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥90% (HPLC)

powder

Calbiochem^®

OK to freeze
protect from light

off-white

DMSO: 5 mg/mL

ambient

−20℃

250 μg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1